Adapalene-loaded poly(ε-caprolactone) microparticles: Physicochemical characterization and in vitro penetration by photoacoustic spectroscopy

• DOI: 10.1371/journal.pone.0213625
• Publication Date: 2019-03-21T17:34:31Z
• Authors: Jessica Mendes Nadal; Guilherme dos Anj...; Andressa Novatski; William Roger Mac...; Daniele Toniolo Dias; Fernanda Malaquia...; Amanda Lyra; João Ricardo Roik; Josiane Padilha d...; Aloisi Somer; Paulo Vitor Farago
• Keywords: Science; Polyesters; 02 engineering and technology; Diffusion; Photoacoustic Techniques; Drug Delivery Systems; Spectroscopy, Fourier Transform Infrared; Adapalene; Particle Size; Drug Carriers; Calorimetry, Differential Scanning; Q; R; Water; Membranes, Artificial; Microspheres; 3. Good health; Spectrophotometry; Microscopy, Electron, Scanning; Solvents; Medicine; Emulsions; 0210 nano-technology; Research Article

Adapalene (ADAP) is an important drug widely used in the topical treatment of acne. It is a third-generation retinoid and provides keratolytic, anti-inflammatory, and antiseborrhoic action. However, some topical adverse effects such as erythema, dryness, and scaling have been reported with its commercial formula. In this sense, the microencapsulation of this drug using polyesters can circumvent its topical side effects and can lead to the enhancement of drug delivery into sebaceous glands. The goal of this work was to obtain ADAP-loaded poly(ε-caprolactone) (PCL) microparticles prepared by a simple emulsion/solvent evaporation method. Formulations containing 10 and 20% of ADAP were successfully obtained and characterized by morphological, spectroscopic, and thermal studies. Microparticles presented encapsulation efficiency of ADAP above 98% and showed a smooth surface and spherical shape. Fourier transform infrared spectroscopy (FTIR) results presented no drug-polymer chemical bond, and a differential scanning calorimetry (DSC) technique showed a partial amorphization of the drug. ADAP permeation in the Strat-M membrane for transdermal diffusion testing was evaluated by photoacoustic spectroscopy (PAS) in the spectral region between 225 and 400 nm after 15 min and 3 h from the application of ADAP-loaded PCL formulations. PAS was successfully used for investigating the penetration of polymeric microparticles. In addition, microencapsulation decreased the in vitro transmembrane diffusion of ADAP.